N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺

生物活性靶点体外研究体内研究 N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺试剂级价格

CAS号:211311-95-4
英文名:N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonaMide
中文名:N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺
CBNumber:CB42640286
分子式:C19H22N2O2S
分子量:342.46
MOL File:211311-95-4.mol

N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺化学性质

沸点 :519.0±60.0 °C(Predicted)
密度 :1.19±0.1 g/cm3(Predicted)
储存条件 :Sealed in dry,Room Temperature
溶解度 :DMF: 15mg/mL; DMSO: 15mg/mL; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL; Ethanol: 3mg/mL
形态 :A solid
酸度系数(pKa) :11.24±0.40(Predicted)
颜色 :White to off-white

N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺性质、用途与生产工艺

生物活性 LY-404187 是有效的，选择性和中枢活性的 AMPA 受体的正变构调节剂，作用于 GluR1i，GluR2i，GluR2o，GluR3i 和 GluR4i 的 EC50 值分别为 5.65、0.15、1.44、1.66 和 0.21 µM。LY-404187 有潜力用于许多精神疾病和神经退行性疾病的研究。
靶点

EC50: 5.65 µM (GluR1i), 0.15 µM (GluR2i), 1.44 µM (GluR2o), 1.66 µM (GluR3i), 0.21 µM (GluR4i)
体外研究

LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells.
LY-404187 (0.03-10 µM) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC ₅₀ =1.3±0.3 µM) and efficacy (E _max =45.3±8.0-fold increase) .
LY-404187 does not affect the magnitude or time course of wholecell K ⁺ or Na ⁺ currents in pre frontal cortex (PFC) pyramidal neurons at concentrations of 10 µM.

体内研究

LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent MPTP-induced neurotoxicity in mice.
LY-404187 (0.5 mg/kg; s.c. for 28 days) attenuates apomorphine-induced contraversive rotations and affords significant protection against the loss of tyrosine hydroxylase positive nigral cell bodies.
LY-404187 (0.1 or 0.5 mg/kg; s.c. for 14 days) affords functional, neurochemical and histological protection after infusion of 6-hydroxydopamine into the substantia nigra in rats.
LY-404187 (0.5 mg/kg; s.c. for 14 days) delayed treatment provides functional and histological improvement, suggesting a trophic action as administration is initiated after cell death.
LY-404187 (0.1 and 0.5 mg/kg; s.c. for 14 days) increases GAP-43 immunoreactivity in the striatum in a dose-dependent manner.

Animal Model:	Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8
Dosage:	0.5 mg/kg
Administration:	S.c; twice daily on weekdays and once daily at weekends for 11 days
Result:	Attenuated the loss of tyrosine hydroxylase immunoreactivity in the substantia nigra. No significant change in tyrosine hydroxylase immunoreactivity in the dorsal and ventral striatum.